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Glucagon was described as an insulin secretagogue as early
2022-07-21

Glucagon was described as an insulin secretagogue as early as 1965 (Samols et al., 1965). Our studies extend these findings by demonstrating that this is a direct effect mediated by distinct receptors in the mouse pancreas. Previous experiments on isolated β OSI-930 clearly show that glucagon is ca
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br NLS and NES Mapping
2022-07-21

NLS and NES Mapping Sequence Comparison of Gli NLSs—NLSs in ZF Domains Alignment of the Gli NLSs of representative metazoan animals suggests that the amino ribosomal s6 kinase residues in the ZF domains are strongly conserved (Figure 4.2, Figure 4.3B). However, the length of the intervening a
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The regulation of the stem cell compartment
2022-07-21

The regulation of the stem cell compartment in CML is dynamic, in particular, during disease progression to a blast crisis and might involve a complex cross-regulation of Hh, Wnt, Notch, and hox signaling pathways (). Significant upregulation of Ptch1 and cyclin D1, upon other proteins, marks the bl
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To directly address whether pharmacological attenuation of p
2022-07-21

To directly address whether pharmacological attenuation of physiological GIP provides therapeutic benefits in obese mice, we pursued a selective long-acting antagonist to complement the work we report on GIPR agonism. We report a GIP analog of sufficient aqueous solubility that employs a shortened N
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JNJ-10198409 sale Discrepancies in the reported results and
2022-07-21

Discrepancies in the reported results and conclusions from different groups regarding studies in ghrelin−/− and ghsr−/− mice are likely explained by the mixed background of the mutant mice used in the different studies [35]; although in the case of mice exposed to HFD, exposure to a HFD immediately
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The suboptimal trypsin selectivity profile of DPC p
2022-07-21

The suboptimal trypsin selectivity profile of DPC423 prompted us to investigate additional P moieties for potency and selectivity. Glycinamide P () showed low nanomolar binding affinity against fXa which suggested that this P moiety sits deeper into the S pocket of fXa. To further elaborate on this
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Another strategy adopted to enhance
2022-07-21

Another strategy adopted to enhance the action of endocannabinoids is indirectly through blocking their metabolism. Indeed, amplifying the action of anandamide and 2-AG by inhibiting their enzymatic degradation has emerged to develop the endocannabinoid system for medicinal purposes. It is interesti
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The biochemical cell culture activities and properties
2022-07-20

The biochemical, cell culture activities and properties of bicyclic carboxamides are compiled in , with the prototype of the series, 4-fluorobenzyl carboxamide , displaying an antiviral profile comparable to the spirocyclic carboxamide . The introduction of a small hydrophobic methyl () and chlori
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Oltipraz has been shown to inhibit the growth of HCC
2022-07-20

Oltipraz has been shown to inhibit the growth of HCC sh4 and is being evaluated in clinical trials as a potential anti-cancer drug for HCC (Mann et al., 2009; Piton et al., 2005; Yates and Kensler, 2007). The present observation that pre-treatment of tumorigenic liver cells with oltipraz causes a la
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The effect of microtubule inhibitors
2022-07-19

The effect of microtubule inhibitors on HBV infection and replication were reported previously. In the study by Dr. Ai-Long Huang's group, microtubule inhibitors promoted HBV replication in Hep2.2.15 and HepG2-HBV1.1, in which HBV DNA is integrated into the chromosomal DNA (Xu et al., 2015). Integra
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br Introduction Chronic rhinosinusitis with nasal polyps CRS
2022-07-19

Introduction Chronic rhinosinusitis with nasal polyps (CRSwNP), a subgroup of chronic rhinosinusitis (CRS), is a chronic inflammatory condition of the nasal and paranasal sinuses. CRSwNP is characterized by grape-like structures with dense inflammatory infiltrates, loose fibrous Tranexamic Acid
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Notably Cu labeled dimeric exendin subunit which was
2022-07-19

Notably, 64Cu-labeled dimeric exendin-4 subunit, which was designated as 64Cu-Mal2Sar-(exendin-4)2, showed higher tumor uptake than that of the monomeric exendin-4 subunit [245]. Besides the most commonly-used GLP-1R agonists exendin-3 and -4 and their derivatives, exendin (9-39) exhibits strong bin
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br Methods and materials br Results and discussion br Conclu
2022-07-19

Methods and materials Results and discussion Conclusions This is the first study that attempted to isolate, purify and identify the characteristics of GSK2334470 from ginseng. In vitro studies have demonstrated that PGL-1 efficiently suppressed SH-SY5Y cell apoptosis induced by Aβ25–35, po
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After brain injury adenosine levels rapidly increase in the
2022-07-19

After brain injury, adenosine levels rapidly increase in the brain [9,10]. As shown in our previous studies, the increased adenosine concentration acts on adenosine A2A receptors (A2ARs), increasing post-traumatic glutamate levels in the brain and exacerbating the severity of injuries [11,12]. Accor
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TH-302 sale br Methods br Results br Discussion Significant
2022-07-19

Methods Results Discussion Significant alterations in the expression of genes related to the glutamatergic system have been shown in several experimental models of epilepsy; however, in most studies focused on acute changes or modifications in expression, these were investigated during the
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